99mTc-3PRGD2 is a new SPECT radiotracer for several tumor imaging with high uptake where integrinαvβ3 is highly expressed.This pilot study was to assess the safety,biodistribution and radiation dosimetry of 9,mTc-3P...99mTc-3PRGD2 is a new SPECT radiotracer for several tumor imaging with high uptake where integrinαvβ3 is highly expressed.This pilot study was to assess the safety,biodistribution and radiation dosimetry of 9,mTc-3PRGD2 in healthy volunteers.The 10 healthy male volunteers were injected with 99mTc-3PRGD2（786.7±55.8 MBq,19.1-24.2 mCi）.Baseline measurements of vital signs,laboratory safety tests and 12-lead electrocardiogram were recorded before and after injection.Blood and urine samples were collected and radiation counts were obtained at various time points.Whole-body scans and ROIs of identified organs were used for visual analysis and estimating the radiation dosimetry.No adverse reactions were found during the study.99mTc-3PRGD2 exhibited a rapid clearance from the blood with less than 45%of the initial dosage at 10 min after injection and gradual increasing radioactivity in urine with（52.9±6）%of original dose at 1440 min.The whole-body imaging showed high radioactive accumulation in bladder.And the highest 99mTc-3PRGD2 uptake was found in the kidneys(3.50×10-2 mSv/MBq).The 99mTc-3PRGD2 exhibited good pharmacokinetic properties and little radiation burden.This study showed that 99mTc-3PRGD2 would be a safe and attractive SPECT agent in clinic applications.展开更多
In recent years,several RGD(Arg-Gly-Asp)-based radiotracers have already been successfully tested in human for the visualization of integrin αvβ3,demonstrating its feasibility in tumor diagnosis.In this paper,we eva...In recent years,several RGD(Arg-Gly-Asp)-based radiotracers have already been successfully tested in human for the visualization of integrin αvβ3,demonstrating its feasibility in tumor diagnosis.In this paper,we evaluated the 99mTc-3P4-RGD2 single photon emission computed tomography/computerized tomography(SPECT/CT)in patients suffering from space occupying disease of esophagus.40 patients(34 males and 6 female;mean age: 58.3 years) with a suspected space occupying lesion of esophagus were included,thus finally obtaining their definite pathologic diagnosis(malignant,n=32;benign,n=8).All patients underwent endoscopic,barium esophagography and SPECT/CT imaging preoperatively.The chest SPECT was performed at 4 h after administration of99mTc-3P4-RGD2 with a dose of 939±118 MBq.The diagnosis precision,sensitivity and specificity among these methods were compared.The relationship between radioactive uptake and clinical pathological stage of esophageal carcinoma was discussed by calculating the tumor to normal esophagus(T/N).Meanwhile,the integrin αvβ3 expression was assessed immunohistochemically in postoperative esophageal tissues.31 patients were diagnosed as esophageal carcinoma;and 1,leiomyosarcoma;and 6.leimyoma;and 2,esophageal tuberculosis.The accuracy,sensitivity and specificity of barium esophagography,endoscopic and SPECT/CT imaging are 92.5/93.8/87.5%,97.5/96.9/100%,and 90/90.6/87.5%,respectively.Abnormal accumulation of radiotracer in 29 malignant lesions is observed.The SPECT/CT imaging displayed the region of radioactive uptake and lesions matched extremely with the T/N ratio from 1.31 to 2.79(mean 2.04).A case with pulmonary metastases and a case with mediastinal lymph node metastases were found which were missed by barium esophagography and endoscopic.The99mTc-3P4-RGD2 uptake of the esophageal carcinoma masses had no relevance to the tumor pathologic classification(P>0.05).There was a significant positive correlation between T/N ratio and positive cell percentage of integrin αvβ3(r=0.976),demonstrating the certain clinical potential in the diagnosis of esophageal carcinoma.展开更多
An overt phenotype of aquaporin-1 knockout（AQP1 ko） mice is growth retardation, suggesting possible defects in bone development and metabolism. In the present study, we analyzed the bone mineral density（ BMD）, bon...An overt phenotype of aquaporin-1 knockout（AQP1 ko） mice is growth retardation, suggesting possible defects in bone development and metabolism. In the present study, we analyzed the bone mineral density（ BMD）, bone calcium and phosphorus contents, and bone metabolism in an AQP1 ko mouse model. The BMD of femurs in AQP1 ko mice was significantly lower than that of litter-matched wildtype mice as measured by dual energy X-ray absorptiometry. Consistently, the contents of bone total calcium and phosphorus were also significantly lower in AQP1 ko mice. The reduced BMD caused by AQP1 deficiency mainly affect male mice. Bone metabolic activity, as indicated by 99m^Tc-MDP absorption measurements, was remarkably reduced in AQP1 ko mice. These results provide the first evidence that AQP1 play an important role in bone structure and metabolism.展开更多
The 99mTc-3PRGD2 targeted SPECT/CT scanning was of significance in detecting differentiated glioma.In this work,the diagnostic value of 99mTc-3PRGD2 scintigraphy in brain glioma was evaluated by the ten clinically ver...The 99mTc-3PRGD2 targeted SPECT/CT scanning was of significance in detecting differentiated glioma.In this work,the diagnostic value of 99mTc-3PRGD2 scintigraphy in brain glioma was evaluated by the ten clinically verified brain glioma patients after obtaining informed consent.The patients first accepted X-ray imaging to localize the detecting regions before administrating with 99mTc-3PRGD2 at a mean radioactivity of 849±115 MBq via single intravenous bolus injection 2 h prior to SPECT/CT imaging.Tumor samples for detectingαvβ3 were collected by surgical operations two weeks after the scintigraphy.The results of CT and SPECT scanning were merged and compared.The correlation between tumor occupation（T/N ratio） andαvβ3 expression level were analyzed.The T/N ratios in brain glioma were proportionally correlated to av(33 positive cell percentage（R2=0.9253,p<0.05）.This study primarily evaluated the clinical application of 99mTc-3PRGD2 SPECT scintigraphy on brain glioma.The more pathological types and detecting strategies covering a large amount of samples would aid to clarify the potentials.展开更多
基金Supported by the National Natural Science Foundation of China(NSFC) projects(no.81271606)the Research Fund of Science and Technology Department of Jilin Province(no.201015185 and no.201201041)the Research Fund of Shenzhen Sci-tech Department of Guangdong Province(no.201102154)
文摘99mTc-3PRGD2 is a new SPECT radiotracer for several tumor imaging with high uptake where integrinαvβ3 is highly expressed.This pilot study was to assess the safety,biodistribution and radiation dosimetry of 9,mTc-3PRGD2 in healthy volunteers.The 10 healthy male volunteers were injected with 99mTc-3PRGD2（786.7±55.8 MBq,19.1-24.2 mCi）.Baseline measurements of vital signs,laboratory safety tests and 12-lead electrocardiogram were recorded before and after injection.Blood and urine samples were collected and radiation counts were obtained at various time points.Whole-body scans and ROIs of identified organs were used for visual analysis and estimating the radiation dosimetry.No adverse reactions were found during the study.99mTc-3PRGD2 exhibited a rapid clearance from the blood with less than 45%of the initial dosage at 10 min after injection and gradual increasing radioactivity in urine with（52.9±6）%of original dose at 1440 min.The whole-body imaging showed high radioactive accumulation in bladder.And the highest 99mTc-3PRGD2 uptake was found in the kidneys(3.50×10-2 mSv/MBq).The 99mTc-3PRGD2 exhibited good pharmacokinetic properties and little radiation burden.This study showed that 99mTc-3PRGD2 would be a safe and attractive SPECT agent in clinic applications.
基金Supported by National Natural Science Foundation of China(NSFC)projects(No.81271606)Research Fund of Science and Technology Department of Jilin Province(No.201015185 and No.201201041)the Research Fund of Shenzhen Sci-tech Department of Guangdong Province(No.201102154)
文摘In recent years,several RGD(Arg-Gly-Asp)-based radiotracers have already been successfully tested in human for the visualization of integrin αvβ3,demonstrating its feasibility in tumor diagnosis.In this paper,we evaluated the 99mTc-3P4-RGD2 single photon emission computed tomography/computerized tomography(SPECT/CT)in patients suffering from space occupying disease of esophagus.40 patients(34 males and 6 female;mean age: 58.3 years) with a suspected space occupying lesion of esophagus were included,thus finally obtaining their definite pathologic diagnosis(malignant,n=32;benign,n=8).All patients underwent endoscopic,barium esophagography and SPECT/CT imaging preoperatively.The chest SPECT was performed at 4 h after administration of99mTc-3P4-RGD2 with a dose of 939±118 MBq.The diagnosis precision,sensitivity and specificity among these methods were compared.The relationship between radioactive uptake and clinical pathological stage of esophageal carcinoma was discussed by calculating the tumor to normal esophagus(T/N).Meanwhile,the integrin αvβ3 expression was assessed immunohistochemically in postoperative esophageal tissues.31 patients were diagnosed as esophageal carcinoma;and 1,leiomyosarcoma;and 6.leimyoma;and 2,esophageal tuberculosis.The accuracy,sensitivity and specificity of barium esophagography,endoscopic and SPECT/CT imaging are 92.5/93.8/87.5%,97.5/96.9/100%,and 90/90.6/87.5%,respectively.Abnormal accumulation of radiotracer in 29 malignant lesions is observed.The SPECT/CT imaging displayed the region of radioactive uptake and lesions matched extremely with the T/N ratio from 1.31 to 2.79(mean 2.04).A case with pulmonary metastases and a case with mediastinal lymph node metastases were found which were missed by barium esophagography and endoscopic.The99mTc-3P4-RGD2 uptake of the esophageal carcinoma masses had no relevance to the tumor pathologic classification(P>0.05).There was a significant positive correlation between T/N ratio and positive cell percentage of integrin αvβ3(r=0.976),demonstrating the certain clinical potential in the diagnosis of esophageal carcinoma.
基金Supported by the National Natural Science Foundation of China(Nos30470405 and 30670477)National Natural ScienceFund for Distinguished Young Scholars(No30325011)+1 种基金Distinguished Young Scholars Fund of Jilin Province(No20030112)Excellent Young Tea
文摘An overt phenotype of aquaporin-1 knockout（AQP1 ko） mice is growth retardation, suggesting possible defects in bone development and metabolism. In the present study, we analyzed the bone mineral density（ BMD）, bone calcium and phosphorus contents, and bone metabolism in an AQP1 ko mouse model. The BMD of femurs in AQP1 ko mice was significantly lower than that of litter-matched wildtype mice as measured by dual energy X-ray absorptiometry. Consistently, the contents of bone total calcium and phosphorus were also significantly lower in AQP1 ko mice. The reduced BMD caused by AQP1 deficiency mainly affect male mice. Bone metabolic activity, as indicated by 99m^Tc-MDP absorption measurements, was remarkably reduced in AQP1 ko mice. These results provide the first evidence that AQP1 play an important role in bone structure and metabolism.
基金Supported by the National Natural Science Foundation of China projects(No.81271606)the Research Fund of Science and Technology Department of Jilin province(No.200705327,No.201015185,and No.201201041)the Research Fund of Shenzhen Sci-tech Department of Guangdong province (No.201102154)
文摘The 99mTc-3PRGD2 targeted SPECT/CT scanning was of significance in detecting differentiated glioma.In this work,the diagnostic value of 99mTc-3PRGD2 scintigraphy in brain glioma was evaluated by the ten clinically verified brain glioma patients after obtaining informed consent.The patients first accepted X-ray imaging to localize the detecting regions before administrating with 99mTc-3PRGD2 at a mean radioactivity of 849±115 MBq via single intravenous bolus injection 2 h prior to SPECT/CT imaging.Tumor samples for detectingαvβ3 were collected by surgical operations two weeks after the scintigraphy.The results of CT and SPECT scanning were merged and compared.The correlation between tumor occupation（T/N ratio） andαvβ3 expression level were analyzed.The T/N ratios in brain glioma were proportionally correlated to av(33 positive cell percentage（R2=0.9253,p<0.05）.This study primarily evaluated the clinical application of 99mTc-3PRGD2 SPECT scintigraphy on brain glioma.The more pathological types and detecting strategies covering a large amount of samples would aid to clarify the potentials.
